Additional Hetero Ring Attached Directly Or Indirectly To The Quinazoline Ring System By Nonionic Bonding Patents (Class 514/266.2)
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Patent number: 9139577Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.Type: GrantFiled: June 26, 2014Date of Patent: September 22, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Andreas Blum, Dirk Gottschling, Armin Heckel, Joerg P. Hehn, Bernhard Schmid, Dieter Wiedenmayer
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Patent number: 9090568Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.Type: GrantFiled: March 12, 2012Date of Patent: July 28, 2015Assignee: IMPACT Therapeutics, Inc.Inventors: Dong Liu, Minsheng Zhang, Kan He, Lianshan Zhang
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Patent number: 9062028Abstract: Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: GrantFiled: April 27, 2012Date of Patent: June 23, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Jun Li, Lawrence J. Kennedy, Steven J. Walker, Haixia Wang, William N. Washburn, Saleem Ahmad, Khehyong Ngu
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Patent number: 9045437Abstract: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R7, R8, R2?, R3?, R4?, R5?, R6?, R7?, R8? independently represent H, OH, F, Cl, Br methoxyl group, NH2 group or NMe2 group; X represents NH, O or S; R6 is selected from the group consisting of: piperidinyl group, morpholino group, methoxyl group, and dimethylamine group. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.Type: GrantFiled: July 30, 2013Date of Patent: June 2, 2015Assignee: China Medical UniversityInventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen, Yang-Chang Wu
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Patent number: 9040548Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3, wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3, wherein R3 is as defined herein; 3) C2-5alkynylR3, wherein R3 is as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: January 3, 2014Date of Patent: May 26, 2015Assignee: AstraZeneca ABInventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
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Publication number: 20150141400Abstract: The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 24, 2013Publication date: May 21, 2015Inventors: Takeshi Murata, Hatsuo Kawada, Satoshi Niizuma, Sousuke Hara, Kihito Hada, Hideaki Shimada, Hiroshi Tanaka, Toshiyuki Mio
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Patent number: 9034886Abstract: The present invention provides a 4-aminoquinazoline derivative having the chemical structure of the following formula, and the use thereof. It is demonstrated by the pharmacological experiment that, the compound or a salt thereof according to the present invention not only has distinct inhibitory effect on histone deacetylases, but also has stronger differentiation induction and anti-proliferative activities for certain tumor cells. It can be used in the treatment of cancers and diseases related to cell differentiation and proliferation. Excellent efficacy is observed especially for leukemia and a solid tumor. As demonstrated by the animal test, the compound or a salt thereof according to the present invention is less toxic.Type: GrantFiled: May 10, 2012Date of Patent: May 19, 2015Assignees: Shanghai Institute of Pharmaceutical Industry, Jiangsu Hengyi Pharmaceutical Co., Ltd.Inventors: Jianqi Li, Qingwei Zhang, Wangping Cai
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Publication number: 20150119405Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.Type: ApplicationFiled: October 23, 2014Publication date: April 30, 2015Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
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Publication number: 20150110723Abstract: The disclosure relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidases (Nox enzymes) and/or myeloperoxidase.Type: ApplicationFiled: May 28, 2013Publication date: April 23, 2015Applicant: EMORY UNIVERSITYInventors: John David Lambeth, Thota Ganesh, Susan M. Smith, Aiming Sun
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Patent number: 9006256Abstract: The present invention provides pharmaceutical compositions and therapeutic methods for treating diseases such as multiple endocrine neoplasia type IIA, multiple endocrine neoplasia type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract. The therapeutic methods and pharmaceutical compositions use a RET kinase inhibiting substance, such as 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and pharmacologically acceptable salts thereof, and involve a step of administering the RET kinase inhibiting substance to a patient.Type: GrantFiled: April 8, 2011Date of Patent: April 14, 2015Assignee: Eisai R&D Management Co., Ltd.Inventor: Junji Matsui
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Publication number: 20150087663Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not limited to leukemias and solid tumors, in mammals, especially humans.Type: ApplicationFiled: September 17, 2014Publication date: March 26, 2015Applicants: SUNSHINE LAKE PHARMA CO., LTD., CALITOR SCIENCES, LLCInventors: Ning Xi, Liang Wang, Zuping Wu, Xuejin Feng, Yanjun Wu
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Patent number: 8987284Abstract: Disclosed are novel quinazoline derivatives containing phosphorus substitutions and methods for the treatment of hyperproliferative diseases (e.g. cancer) using the compounds. These compounds are type I receptor protein kinase inhibitors useful in treating disorders related to abnormal protein kinase activities such as cancer and inflammation in mammals. Also disclosed are pharmaceutical compositions containing the compounds, methods for the preparation of the compounds and their pharmaceutically acceptable salts.Type: GrantFiled: July 2, 2010Date of Patent: March 24, 2015Assignee: Newgen Therapeutics, Inc.Inventors: Wang Shen, Aimin Zhang, Junfa Fan, Xiaoling Zheng
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Patent number: 8987285Abstract: The present invention relates to a novel crystalline anhydrous form of [(5-chlorothiophene-2-ylsulfonylcarbamoyl)-(4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)phenyl)amide, potassium salt, and its use in the treatment or prevention of a condition or a disorder with platelet ADP receptor inhibition, in particular, P2Y12 inhibition, in animals, particularly humans. It also relates processes for making such a novel crystalline form. The present invention also relates to a solid, oral formulation of this novel crystalline form, its preparation and use thereof.Type: GrantFiled: December 5, 2011Date of Patent: March 24, 2015Assignee: Portola Pharmaceuticals, Inc.Inventors: Ulrich Meier, Nicole Bieri, Dieter Becker, Julien Taillemite, Marie-Pierre Filliot, Tanja Meister
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Publication number: 20150072955Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.Type: ApplicationFiled: October 14, 2014Publication date: March 12, 2015Applicant: Resverlogix Corp.Inventor: Henrik C. Hansen
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Publication number: 20150057260Abstract: The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: August 22, 2014Publication date: February 26, 2015Applicant: Genentech, Inc.Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Xingyu Lin, Jason Burch
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Publication number: 20150050239Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: July 19, 2013Publication date: February 19, 2015Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Patent number: 8957073Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: May 11, 2011Date of Patent: February 17, 2015Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
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Publication number: 20150045323Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.Type: ApplicationFiled: September 13, 2013Publication date: February 12, 2015Inventors: Linda N. Casillas, Pamela A. Haile, Robert W. Marquis, JR., Gren Wang
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Patent number: 8952022Abstract: The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.Type: GrantFiled: July 22, 2011Date of Patent: February 10, 2015Assignee: Generics [UK] LimitedInventors: Vinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
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Publication number: 20150025072Abstract: The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula (I).Type: ApplicationFiled: October 7, 2014Publication date: January 22, 2015Applicant: PRANA BIOTECHNOLOGY LIMITEDInventors: Penelope Jane HUGGINS, Jack Gordon PARSONS
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Publication number: 20150025091Abstract: The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.Type: ApplicationFiled: September 18, 2014Publication date: January 22, 2015Applicant: ASTRAZENECA ABInventor: James MCCABE
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Publication number: 20150010545Abstract: The present invention provides a method of treating breast cancer that is nonresponsive to treatment with trastuzumab, comprising administering to a subject in need of such treatment a therapeutically effective amount of compound N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 27, 2012Publication date: January 8, 2015Inventors: Samuel Waksal, Lillian Chiang
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Patent number: 8927530Abstract: The present invention provides a combination comprising (a) a compound of formula (I) and (b) one or more antineoplastic agents selected from the group consisting of an antimetabolite agent, analkylating or alkylating-like agent, an intercalating agent, a topoisomerase I or II inhibitor, an antimitotic agent, a kinase inhibitor, a proteasome inhibitor and an antibody inhibiting a growth factor or its receptor, wherein active ingredients of the combination are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate or solvate thereof, useful in the treatment of tumors.Type: GrantFiled: May 21, 2010Date of Patent: January 6, 2015Assignee: Nerviano Medical Sciences S.R.L.Inventors: Barbara Valsasina, Italo Beria, Antonella Ciavolella, Dario Ballinari, Enrico Pesenti, Juergen Moll, Mara Emanuela Casnaghi, Alessandro Luciano Croci
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Publication number: 20150005278Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.Type: ApplicationFiled: June 26, 2014Publication date: January 1, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Andreas BLUM, Dirk GOTTSCHLING, Armin HECKEL, Joerg P. HEHN, Bernhard SCHMID, Dieter WIEDENMAYER
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Publication number: 20140378475Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: June 25, 2014Publication date: December 25, 2014Inventors: Douglas G. Batt, Myra Beaudoin Bertrand, George Delucca, Michael A. Galella, Soo Sung Ko, Charles M. Langevine, Qingjie Liu, Qing Shi, Anurag S. Srivastava, Joseph A. Tino, Scott Hunter Watterson
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Patent number: 8916576Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.Type: GrantFiled: December 14, 2012Date of Patent: December 23, 2014Assignee: Surface Logix, Inc.Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Brian Kirk, Siya Ram, Paul Sweetnam, Hemalatha Seshadri
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Patent number: 8916574Abstract: The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.Type: GrantFiled: September 20, 2010Date of Patent: December 23, 2014Assignee: Qilu Pharmaceutical Co., Ltd.Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Zhongru Guo, Ying Li, Shaobo Yang, Shousheng Yan, Jianrong Zhu, Qingmin Yang, Minghui Zhang
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Patent number: 8916575Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.Type: GrantFiled: May 18, 2012Date of Patent: December 23, 2014Assignee: Janssen R&D IrelandInventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
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Patent number: 8916554Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: July 22, 2013Date of Patent: December 23, 2014Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
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Patent number: 8906931Abstract: The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.Type: GrantFiled: August 28, 2014Date of Patent: December 9, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Waldemar Pfrengle, Guenther Huchler, Markus Ostermeier, Peter Sieger
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Patent number: 8906930Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R4 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: October 26, 2010Date of Patent: December 9, 2014Assignee: Merck Patent GmbHInventors: Hans Michael Eggenweiler, Christian Sirrenberg, Hans Peter Buchstaller
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Patent number: 8901138Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined herein, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.Type: GrantFiled: November 7, 2013Date of Patent: December 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Andreas Blum, Dirk Gottschling, Armin Heckel, Joerg Hehn, Thorsten Lehmann-Lintz, Dieter Wiedenmayer
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Publication number: 20140349992Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Applicant: Sunovion Pharmaceuticals Inc.Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
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Patent number: 8889698Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.Type: GrantFiled: September 23, 2011Date of Patent: November 18, 2014Assignee: Resverlogix Corp.Inventor: Henrik C. Hansen
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Patent number: 8883809Abstract: The present invention provides a compound of general formulae 3a-i to 6a-i, 7a-i to 10a-i, 12a-i to 15a-i, 16a-i to 19a-i, 21a-i to 24a-i, 25a-i to 28a-i, 30a-i to 33a-i, 34a-i to 37a-i and 39a-i to 42a-i, 43a-i to 46a-i useful as potential antitumour agents against human cancer cell lines and a process for the preparation thereof.Type: GrantFiled: September 8, 2009Date of Patent: November 11, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Ahmed Kamal, Earla V. Bharathi, Jonnala S. Reddy, Dudekula Dastagiri, Arutla Viswanath
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Publication number: 20140315886Abstract: Methods of treating disorders using compounds (I) that modulate stri-atal-enriched tyrosine phosphatase (STEP) are described herein. Exemplary disorders include schizophrenia and cognitive deficit. Formula (I).Type: ApplicationFiled: June 28, 2012Publication date: October 23, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Masaki Suzuki, Kazumi Kondo, Muneaki Kurimura, Krishna Reddy Valluru, Akira Takahahi, Takeshi Kuroda, Haruka Takahashi, Tae Fukushima, Shin Miyamura, Indranath Ghosh, Abhishek Dogra, Geraldine Harriman, Amy Elder, Satoshi Shimiza, Kevin J. Hodgetts, Jason S. Newcom
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Patent number: 8865708Abstract: Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof.Type: GrantFiled: May 6, 2011Date of Patent: October 21, 2014Assignees: California Institute of Technology, The University of Kansas, Cleave Biosciences, Inc.Inventors: Raymond J. Deshaies, Tsui-Fen Chou, Frank J. Schoenen, Kelin Li, Kevin J. Frankowski, Jeffrey Aube, Samuel W. Gerritz, Han-Jie Zhou
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Patent number: 8865704Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: GrantFiled: October 6, 2010Date of Patent: October 21, 2014Assignee: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
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Publication number: 20140309190Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: June 17, 2014Publication date: October 16, 2014Applicant: BIOGEN IDEC MA INC.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Ma Bin, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Publication number: 20140309184Abstract: Embodiments of the present disclosure relate to methods and compositions for treating a subject with ovarian cancer. Some embodiments include treating a subject with a particular combination of chemotherapeutic agents.Type: ApplicationFiled: July 20, 2012Publication date: October 16, 2014Applicant: UNIVERSITY OF SOUTH ALABAMAInventors: Rodney P. Rocconi, Lalita Samant
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Publication number: 20140309245Abstract: The invention provides novel heterocyclic carboxamide compounds compounds according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: December 17, 2012Publication date: October 16, 2014Inventors: Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Ruoxi Lan, Lizbeth Celeste De Selm, Constantin Neagu, Justin Potnick, Srinivasa R. Karra, Theresa L. Johnson
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Patent number: 8859570Abstract: The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.Type: GrantFiled: December 23, 2009Date of Patent: October 14, 2014Assignee: AstraZeneca ABInventor: James McCabe
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Patent number: 8859571Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, and methods of making and using the same.Type: GrantFiled: November 1, 2010Date of Patent: October 14, 2014Assignee: GlaxoSmithKline LLCInventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp
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Patent number: 8853225Abstract: The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.Type: GrantFiled: January 27, 2012Date of Patent: October 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Waldermar Pfrengle, Guenther Huchler, Markus Ostermeier, Peter Sieger
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Publication number: 20140296230Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4 and A1 to A5 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: March 26, 2014Publication date: October 2, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christian SMETHURST, Harald ENGELHARDT, Davide GIANNI, Ulrich REISER
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Patent number: 8846700Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).Type: GrantFiled: September 9, 2013Date of Patent: September 30, 2014Assignee: MSD K.K.Inventors: Tomoharu Iino, Akio Ohno, Norikazu Otake, Takuya Suga, Masanori Asai
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Patent number: 8846699Abstract: The present invention relates to a novel quinazoline derivative compound having the formula (1) as follows: with the constituents defined in claim 1, and a pharmaceutically acceptable salt thereof as a multiplex inhibitor, a method for the preparation thereof, and a pharmaceutical composition and a therapeutic composition comprising same as an active ingredient. The inventive quinazoline derivative as a multiplex inhibitor can selectively and effectively inhibit diseases caused by the overactivity of a tyrosine kinase.Type: GrantFiled: November 8, 2006Date of Patent: September 30, 2014Assignee: Hanmi Pharm. Co., Ltd.Inventors: Young-Gil Ahn, Jong Woo Kim, Keuk Chan Bang, Bum Woo Park, Se Young Kim, Kyungik Lee, Kyuhang Lee, Myoung-Sil Ko, Han Kyong Kim, Young Hoon Kim, Maeng Sup Kim, Gwan Sun Lee
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Patent number: 8846654Abstract: A subject-matter of the present invention is the use of compounds of formula (I) in the base, hydrate or solvate form or in the form of their mixtures, as medicaments or for the preparation of medicaments intended for the treatment of at least one cardiovascular disease and/or to prevent the appearance of at least one cardiovascular disease.Type: GrantFiled: October 7, 2011Date of Patent: September 30, 2014Assignee: SanofiInventors: Philip Janiak, Gilbert Marciniak, Jean-Francois Nave, Fabrice Viviani
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Publication number: 20140288048Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20140288100Abstract: Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal.Type: ApplicationFiled: September 23, 2011Publication date: September 25, 2014Applicants: University of Utah Research Foundation, The United States of American, as Represented by the Decretary, Department of Health and HumanInventors: Matthew B. Boxer, Martin J. Walsh, Li Liu, Cordelle D. Tanega, Min Shen, Kent Lai, Manshu Tang, Douglas S. Auld